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TAK-220

CAS No. : 333994-00-6

Biological Activity：TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC₅₀s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC₅₀s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC₉₀s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.

Research Area：Infection|Endocrinology

Targets：HIV|CCR

Related Screening Libraries:Bioactive Compound Library Plus;

Related Small Molecules:HIV-1 TAT (48-60);Seletracetam lithium;HIV-IN-2;Triptonine B;LMD-009;FC131;Peritassine A;PF-04634817 succinate;Flavopiridol;TAT (48-57);FGI-106 tetrahydrochloride;(Z)-9-Propenyladenine;Apabetalone;Decanoyl-RVKR-CMK TFA;ONX-0914 TFA;Apelin-36(rat, mouse);Ulonivirine;Islatravir

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